Abstract
Chemical investigation of secondary metabolites from the marine-derived fungus Aspergillus austroafricanus Y32-2 resulted in the isolation of two new prenylated indole alkaloid homodimers, di-6-hydroxydeoxybrevianamide E (1) and dinotoamide J (2), one new pteridine alkaloid asperpteridinate A (3), with eleven known compounds (4–14). Their structures were elucidated by various spectroscopic methods including HRESIMS and NMR, while their absolute configurations were determined by ECD calculations. Each compound was evaluated for pro-angiogenic, anti-inflammatory effects in zebrafish models and cytotoxicity for HepG2 human liver carcinoma cells. As a result, compounds 2, 4, 5, 7, 10 exhibited pro-angiogenic activity in a PTK787-induced vascular injury zebrafish model in a dose-dependent manner, compounds 7, 8, 10, 11 displayed anti-inflammatory activity in a CuSO4-induced zebrafish inflammation model, and compound 6 showed significant cytotoxicity against HepG2 cells with an IC50 value of 30 µg/mL.
Highlights
The ocean has the characteristics of high salinity, high pressure, low temperature, low oxygen content, and oligotrophic environment, which enables microorganisms to have unique metabolic adaptation mechanisms and produce natural products with novel structures and diverse bioactivities [1]
Many of the NMR signals appeared in pairs, hinting towards structural distinctiveness and complexity
Their structures including the absolute configurations were elucidated by various spectroscopic methods and ECD calculations
Summary
The ocean has the characteristics of high salinity, high pressure, low temperature, low oxygen content, and oligotrophic environment, which enables microorganisms to have unique metabolic adaptation mechanisms and produce natural products with novel structures and diverse bioactivities [1]. A large number of novel secondary metabolites, such as polyketides, alkaloids, terpenes, steroids, peptides, etc., have been discovered from marine-derived Aspergillus species [3], and showed diverse bioactivities like antibacterial, antitumor, antioxidant, and anti-inflammatory activities [4]. More than 80% natural products were directly or indirectly related to small molecule drugs for the treatment of various diseases in the last 30 years, and many marine alkaloids with bioactivities have been comprehensively studied for drug development [5,6]. Mar. Drugs 2021, 19, 98 of 12 ucts were directly or indirectly related to small molecule drugs for the treatment of 2various diseases in the last 30 years, and many marine alkaloids with bioactivities have been comprehensively studied for drug development [5,6]
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